Obesity caused by excessively high caloric intake and accumulation of surplus fat often leads to various types of degenerative diseases. Dieting, bariatrics and cytotherapy is of major concern to patients who suffer from obesity-caused diseases and also to healthy people who, for cosmetic reasons, wish to control their caloric intake and thereby decrease their weight.
Dieting often requires that significant limitations be placed on the amount of caloric intake, and the amount of fat and carbohydrates consumed by an individual are invariably diminished in a successful dietary plan. However, due to the inherent causes of obesity and overeating, dieting by itself is often unsuccessful in achieving the patient's goals. There are two primary reasons for this. First, there is an immense amount of patience required by the dieter to lose significant amounts of weight. Second, and perhaps more important, are the inherent reasons that people eat to excess. For example, it is well known that the vast majority of over-eating is done to satisfy anxiety. Thus, caloric intake often is not engaged in for the purpose of satisfying hunger and meeting metabolic needs, but to satisfy secondary needs in the individual's life.
In the past, appetite suppression has been accomplished by the use of centrally-acting neuro-stimulants such as cocaine, methamphetamine hydrochloride, dextroamphetamine sulfate and other derivatives of the amphetamine molecule. These drugs typically are extremely effective for a short period of time, but tachyphylaxis invariably develops and there are inherent side-effects with the use of such drugs. Other approaches have also been tried without a great deal of success, including a high fiber intake with unmetabolizable foods (such as konjak, also known as glucomannin) and physical methods (such as exercise). Other approaches that have been used include the use of local anesthetics. However, these compounds have proved unsuccessful because they are easily hydrolyzed in the stomach by hydrochloric acid which is secreted by the chief cells in the stomach lining. Injectable cholecystokinin has also been considered as a methodology for decreasing the sensation of appetite, but this method requires intravenous injection on a regular basis.
Accordingly, there is a need in the art for an appetite suppressant which will suppress appetite by exerting a local gastric effect, as well as central effects such as a perceived nutrient overload effect, thereby diminishing appetite for a significant period of time. There is also a need for an appetite suppressant which avoids the development of tachyphylaxis. This invention fulfills these needs, and provides other related advantages.